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Wyniki wyszukiwania dla: acyl meldrum's acid
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Easy formation of acyl-Meldrum's acid anhydride
PublikacjaAcyl Meldrum's acid are usually a good source of ketenes upon definite thermal composition. However we treated acyl-Meldrum's acid with the Lewis acid and we observed formation of 5[[(2,2-dimethyl-4,6-dioxo-1,3-dioxan 5 ylidene)(acyl/arylamino)mathoxy](acyl/arylamino)methylene]-2,2dimethyl-1,3-dioxane-4,6 dione which means acyl-Meldrum's acid anhydride. The chemical properities of acyl-Meldrum's acid anhydride were explored.
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Acyl Meldrum's acid derivatives: application in organic synthesis
PublikacjaThis review is focused on one of the most important classes of Meldrum's acid derivatives commonly known as acyl Meldrum's acids. The preparation methods of these compounds are considered including the recently proposed and rather rarely used ones. The chemical properties of acyl Meldrum's acids are described in detail, including thermal stability and reactions with various nucleiophiles. The possible mechanisms of these transformations...
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The stereoselective formation of β-lactams with acyl ketenes generated from 5-acyl-Meldrum's acids
PublikacjaAcyl ketenes formed during thermal decompositions of 5-acyl-2,2-dimethyl-1,3-dioxa-4,6-diones undergo stereoselective [2+2] cycloaddition to chiral aldimines. We report the first example of optically active 3-acyl-β-lactams formation from Meldrum’s acid derivatives.
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Preparation of Pseudopeptides Building Blocks with Retro-Thioamide Bond Mediated via Thiocarbamoyl Meldrum's Acid
PublikacjaAn easy and efficient synthesis of pseudo tripeptide containing a thiomalonamide moiety was developed. Isothiocyanate derivatives of amino acids react smoothly with 2,2-dimethyl-1,3-dioxane-4,6-dione yielding new thiocarbamoyl Meldrum's acids. Thermal decomposition of this new Meldrum's acid derivatives generate thiocarbamoyl ketenes, which acylate amino acid esters to give pseudo tripeptides.
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TMSCl Promoted Acylation of Amines with 5-(α-amino- α'-hydroxy)methylene Meldrum's Acids - Elucidation of Mechanism.
PublikacjaRecently we have observed accelerating influence of trimethyl silyl chloride addition on the rate of the reactions of 5-(α-amino- α'-hydroxy)methylene Meldrum's Acids with amines, particularly in the case of highly basic amines. However the nature of the aforementioned process remain unexplained. In proposed communication we wish to report insightful elucidation of this mechanism. The reaction under investigation involves simply...
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Tmscl as a rate accelerating additive in acylations of amines with 5-(α-amino- α'-hydroxy)methylene meldrum's acids
PublikacjaAspects are presented of the acylation of amines, alcohols and thiols with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids. We placed special emphasis on the acylation reaction of secondary amines with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids, which, due to their basicity, caused problems concerning salt formation with a Meldrum acid derivative. We found that secondary amines, which react at the slowest rate and with a...
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TMSCL as a rate accelerating additive in acylations of amines with 5-(α- amino-α'-hydroxy)methylene meldrum's acids
PublikacjaAspects are presented of the acylation of amines, alcohols and thiols with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids. We placed special emphasis on the acylation reaction of secondary amines with 5-(α-amino- α'-hydroxy)methylene Meldrum's acids, which, due to their basicity, caused problems concerning salt formation with a Meldrum acid derivative. We found that secondary amines, which react at the slowest rate and with a...
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Synthesis and reactivity of O-acyl selenophosphates
PublikacjaThe synthesis of several new O-acyl selenophosphates were investigated. The stability and reactivity of the products were studied and related to their structure.
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Boron Difluoride Complexes of Carbamoyl Meldrum's Acids
Publikacja5-[Hydroxy(aryl/alkylamino)methylene]-2,2-dimethyl-1,3-dioxane-4,6-diones react with BF3•Et2O in mild conditions leading to the formation of boron difluoride complexes of carbamoyl Meldrum's acids. The X-ray structure has been obtained for one representative complex. The obtained new compounds are fairly stable at standard ambient conditions and easily isolable.
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Configurational and Conformational Preferences in Stereoselective Acylations of N-Methyl-1,3-diaminopropane with Acyl Chlorides
PublikacjaEvidence for a stereoinduction profile of the reaction of N-methyl-1,3-diaminopropane with acyl chlorides was provided. A possibility to engage in intramol. CH2···HN and Cl···H-N interactions and the proton migration process to the methylamino group leads to the E secondary amides carrying the N···H+···N or N-H···N bridges, that show unusual spectroscopic images. Empirical relations between the ΔδC chem. shift differences,...
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A simple access to o-acyl bicyne
PublikacjaW publikacji przedstawiono prostą metodę otrzymywania o-acylowych pochodnych bicyny. Substratem do syntezy była n,n-bis(2-hydroksyetylo)glicyna - bicyna. Bicynę najpierw przeprowadzano w ester benzylowy w reakcji z alkoholem benzylowym i kwasem p-toluenosulfonowym w temp. 75 st. C. Tak otrzymany związek, acylowano kwasami organicznymi w obecności DCC ( dicyklokeksylokarbodiimid)i DMAP (dimetyloaminopirydyna), otrzymując o-acylowe...
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Synthesis and reactivity of O-acyl selenophosphates.
PublikacjaMieszane bezwodniki kwasów monoselenofosforowych >P(Se)O-C(O)- w zależności od podstawników na atomie fosforu oraz karbonylowym atomie węgla izomeryzują do układów Se-mostkowych >P(O)Se-(O)C- oraz ulegają dekarboksylacji (dekarbonylacji i dekarboksylacji) do estrów Se-alkilowych >P(O)Se-. W eksperymantach krzyżowych następuje wzajemna wymiana grup acylowych pomiędzy cząsteczkami bezwodników.
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Synthesis and reactivity of O-acyl selenophosphates
PublikacjaPrzeprowadzono syntezę nowych selenofosforanów acylu. Badano stabilność i reaktywność tych bezwodników w odniesieniu do ich struktury.
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Fatty acyl benzamido antibacterials based on inhibition of DnaK-catalyzed protein folding
PublikacjaWe have reported that the hsp70 chaperone DnaK from Escherichia coli might assist protein folding by catalyzing the cis/trans isomerization of secondary amide peptide bonds in unfolded or partially folded proteins. In this study a series of fatty acylated benzamido inhibitors of the cis/trans isomerase activity of DnaK was developed and tested for antibacterial effects in E. coli MC4100 cells. Nα-[Tetradecanoyl-(4-aminomethylbenzoyl)]-l-asparagine...
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Synthesis and structural investigation of N-acyl selenophosphoramides
PublikacjaN-acylowane amidy kwasu O,O-neopentylidenomonoselenofosforowego, w zależności od podstawnika na atomie azotu, krystalizują jako konformery zawierające selen w pozycji ekwatorialnej bądź aksjalnej. Wyniki tych eksperymentów wyjaśniono działaniem efektu anomerycznego.
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Nucleic Acid Therapeutics
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Hyaluronic acid/tannic acid films for wound healing application
PublikacjaIn this study, thin films based on hyaluronic acid (HA) with tannic acid (TA) were investigated in three different weight ratios (80HA/20TA, 50HA/50TA, 20HA/80TA) for their application as materials for wound healing. Surface free energy, as well as their roughness, mechanical properties, water vapor permeability rate, and antioxidant activity were determined. Moreover, their compatibility with blood and osteoblast cells was investigated....
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublikacjaMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid
PublikacjaThe series of 16 novel amino acid and peptide mycophenolic acid (MPA) derivatives was obtained as potential antibacterial agents. Coupling of MPA with respective amines was optimized with condensing reagents such as EDCI/DMAP and T3P/TEA. Amino acid analogs were received both as methyl esters and also with the free carboxylic group. The biological activity of the products was tested on five references bacterial strains: Klebsiella...
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Thermogravimetrical investigations of the dealkoxycarbonylation of N-acyl-α-triphenylphosphonioglycinates
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Modifications of total synthesis of mycophenolic acid
PublikacjaThe total synthesis of mycophenolic acid (MPA), a potent immunosuppressant, was modified. The obtained mycophenolic acid was suitable for further preparation of new prospective immunosuppressants with improved therapeutic properties.
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New Analogues of Mycophenolic Acid
PublikacjaMycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives of MPA have been used clinically: mycophenolate mofetil (MMF,...
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Molecular geometry of phenylboronic acid
Dane BadawczeData presents molecular geometry of the ground singlet state of phenylboronic acid. The geometry was obtained via DFT calculations using Becke–Lee–Yang–Parr density functional (B3LYP) with the balanced polarized triple-zeta def2-TZVP basis set. Geometry is provided in the XYZ file format.
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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One-step formation of n-alkenyl-malonamides and n-alkenyl-thiomalonamides from carbamoyl meldrum's acids.
PublikacjaA one-pot synthesis for the preparation of N-alkenyl-malonamides and N-alkenyl-thiomalonamides was developed. 5-[Hydroxy/mercapto(aryl/alkylamino)methylene]-2,2-dimethyl-1,3-dioxane-4,6-dione act as a source of ketenes that react with the tautomeric form of alkyl-(2-phenyl-propylidene)-amines. A possible [2+2] or [4+2] cycloaddition product of ketene to imines was not observed.
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Dissociative electron attachment to benzoic acid (C7H6O2)
PublikacjaThe dissociative electron attachment (DEA) to benzoic acid (C6H5COOH) has been studied using an experimental crossed beam setup of a quadrupole mass spectrometer and a trochoidal electron monochromator. Relative partial cross sections for the DEA to produce negative ion fragments show the main channels for dissociation. The comparison of the present results with the ultraviolet photoelectron spectrum of benzoic acid [J. Meeks,...
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ANTISENSE & NUCLEIC ACID DRUG DEVELOPMENT
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Current Protocols in Nucleic Acid Chemistry
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Experimental and Theoretical Study on Electron Interactions with Acetic Acid Molecules
PublikacjaThe absolute total cross section for electron collisions with acetic acid has been measured using an electrostatic electron spectrometerand linear transmission method for collision energies ranging from 0.4 to 300eV. Elastic electron scattering from acetic acid within a low-energy range has also been studied theoretically using the Schwinger multichannel and R-matrix methods, in the static-exchange and static-exchange plus polarization...
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Meldrum’s acid assisted formation of tetrahydroquinolin‑2‑one derivatives a short synthetic pathway to the biologically useful scaffold
PublikacjaA new method for the preparation of tetrahydroquinolin-2-one derivatives is presented. This approach involves a two-step reaction between enaminones and acylating agents, immediately followed by electrophilic cyclization, all within a single synthesis procedure, eliminating the need to isolate intermediates. The entire process is facilitated by the use of acyl Meldrum’s acids which not only shortens the preparation time of the...
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Amino Acid and Peptide‐Based Antiviral Agents
PublikacjaA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Microwave-assisted preparation of potato starch silicated with silicic acid
PublikacjaApplication of microwave irradiation for the silication of granular potato starch with silicic acid, and the properties of silicated starch were investigated. Potato starch was esterified on 20 min microwave irradiation of starch with silicic acid, applying the power of 450 or 800Wand, for comparison, on 120 min convectional heating of the reagent blend at 100 ◦C. The degree of esterification and the reaction efficiency did not...
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Beeswax And Palmitic Acid Utilization With Heat Pipes For Electronics Cooling
PublikacjaThis paper presents an experimental study of heat pipes supported by phase change materials (PCMs) coated at their adiabatic sections in application for electronics cooling. The PCMs investigated in this research were palmitic acid and beeswax, the latter being considered as a more cost-effective alternative. The study focused on three powers: 20W, 25W, and 30W. The experimental results revealed that the incorporation of palmitic...
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Rhodotorulic Acid and its Derivatives: Synthesis, Properties, and Applications
PublikacjaSiderophores are low molecular weight compounds produced by microorganisms to scavenge iron in iron-deficient environments. Rhodotorulic acid (RA), a natural hydroxamate siderophore, plays a vital role in iron acquisition for fungi and bacteria. As the simplest natural hydroxamate siderophore, RA exhibits a high affinity for ferric ions, enabling it to form stable complexes that facilitate iron uptake and transport within microorganisms....
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New conjugates of mycophenolic acid and their antiproliferative activity
PublikacjaThe new conjugates of mycophenolic acid (MPA) were obtained in the reaction of N6-(ω-aminoalkyl)adenosines with MPA in the presence of EDCI as a coupling reagent. New compounds 4a–h were evaluated on leukemia cell line (Jurkat) and PBMC from healthy donors. Length of the linker influenced observed activity. The compound 4b possessing 1,3-diamine spacer exhibited the most promising results and can be considered to further investigations.
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Thermal and mechanical properties of polyurethanes modified with L-ascorbic acid
PublikacjaIn this study we report the thermal and mechanical properties of polyurethanes modified with ascorbic acid (AA). Ascorbic acid was used as a modifier at concentration of 1 or 2 mass%. The antioxidative properties of AA may improve the biocompatibility of the obtained materials, which were designed for biomedical applications. In this paper we describe characterization of obtained unmodified and ascorbic acid modified polyurethanes...
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Physical crosslinking of hyaluronic acid in the presence of phospholipids in an aqueous nano-environment
PublikacjaHyaluronic acid and phospholipids are two components in the synovial joint cavity that contribute to joint lubrication synergistically. Molecular dynamics simulations were performed and hydrogen bonds in hyaluronic acid were analyzed to identify specific sites that are responsible for its physical cross-linking. Two molecular masses of hyaluronic acid, 10 kDa and 160 kDa, were considered. We use molecular dynamics simulations and...
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Maternal smoking Modulates Fatty Acid Profile of Breast Milk
PublikacjaAIM: We hypothesized that the fatty acid composition of breast milk can be affected by a smoking habit in the mother. Consequently, this study verified whether maternal smoking modulates, and if so to what extent, the breast milk fatty acid profile. METHODS: The study included 20 postpartum women who declared smoking more than five cigarettes daily throughout a period of pregnancy and lactation, and 136 non-smoking postpartum women....
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Cytotoxic and Antioxidant Activities of Benzohydroxamic Acid Analogues
Publikacja20 benzohydroxamic acid analogues were synthesized and evaluated for their in vitro cytotoxicities against mouse mammary tumor cells as well as antioxidant activities against DPPH radical and superoxide anion. It was found that benzothiohydroxamic acids exhibit greater cytotoxicities than benzohydroxamic acids and N-isopropyl derivatives are more active than N-methyl ones. On the other hand, benzothiohydroxamic acids show more...
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The profiles and spectrum of aqua solution of tannic acid by HPLC-DAD-MS analysis.
Dane BadawczeThe profiling of tannic acid is determined by examining the content and proportion / ratio of gallotannins [Aras et al. 2016, Clifford et al. 2007, Gauri et al. 2012, Nishizawa et al. 1982]. In order to check the ion mass distribution (TIC) in an aqueous solution of commercial tannic acid, a direct sample injection (TA) was performed into the mass spectrometer....
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An Improved Synthesis of Trisodium (R)-Homocitrate from Citric Acid
PublikacjaA method of synthesis of trisodium (R)-homocitrate starting from citric acid is reported. The procedure affords the final product of high optical purity with satisfactory yield.
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Molecular targets for antifungals in amino acid and protein biosynthetic pathways
PublikacjaFungi cause death of over 1.5 million people every year, while cutaneous mycoses are among the most common infections in the world. Mycoses vary greatly in severity, there are long-term skin (ringworm), nail or hair infections (tinea capitis), recurrent like vaginal candidiasis or severe, life-threatening systemic, multiorgan infections. In the last few years, increasing importance is attached to the health and economic problems...
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Dissociation of 2-oxopropanoic acid by low energy electrons
PublikacjaElectron attachment to molecular target can lead to a variety of negative fragment ions. We experimentally probe the main dissociative electron attachment (DEA) channels in 2-oxopropanoic acid (CH3 - CO - COOH) - an important trace component in the Earth's atmosphere. In our studies we utilise nearly mono-energetic electrons at electron energies from 0 eV up to 15 eV.
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Ab initio study of formic acid monomer, dimer and trimer
PublikacjaConfigurations of the formic acid monomer, dimer and trimer are presented. The total energies for these structures have been calculated while the negatively charged clusters were considered and the possible pathways of interaction of low energy electrons with monomers and clusters were discussed. Calculations have been executed using 6-311 G** and 6-311 ++G** basis sets. The electron affinities of monomer and clusters are presented....
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Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)
PublikacjaThe aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA−PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro...
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Electron attachment and electron iozization of acetic acid clusters embedded in helium nanodroplets
PublikacjaThe effect of incident electrons on acetic acid clusters is explored for the first time. The acetic acid clusters are formed inside liquid helium nanodroplets and both cationic and anionic productsejected in to the gas phase aredetected by mass spectrometry.
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ASCORBIC ACID IN POLYURETHANE SYSTEMS FOR TISSUE ENGINEERING
PublikacjaThe introduction of the paper was devoted to the main items of tissue engineering (TE) and the way of porous structure obtaining as scaffolds. Furthermore, the significant role of the scaffold design in TE was described. It was shown, that properly designed polyurethanes (PURs) find application in TE due to the proper physicochemical, mechanical and biological properties. Then the use of L-ascorbic acid (L-AA) in PUR systems for...
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1-(N-Acylamino)alkyl Sulfones from N-Acyl-α-amino Acids or N-Alkylamides
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